Synthesis and Cytotoxicity Studies of Novel [1,2,4]Triazolo[1,5-a]pyrimidine-7-amines

Xin Zhai; Yan-Fang Zhao; Ya-Jing Liu; Yong Zhang; Feng-Qiang Xun; Jun Liu; Ping Gong

doi:10.1248/cpb.56.941

Regular Articles

Synthesis and Cytotoxicity Studies of Novel [1,2,4]Triazolo[1,5-a]pyrimidine-7-amines

Xin Zhai, Yan-Fang Zhao, Ya-Jing Liu, Yong Zhang, Feng-Qiang Xun, Jun Liu, Ping Gong

Author information

Xin Zhai
Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University
Yan-Fang Zhao
Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University
Ya-Jing Liu
Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University
Yong Zhang
Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University
Feng-Qiang Xun
Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University
Jun Liu
Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University
Ping Gong
Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University

Keywords: [1,2,4]triazolo[1,5-a]pyrimidine-7-amine, synthesis, cytotoxicity

JOURNAL FREE ACCESS

2008 Volume 56 Issue 7 Pages 941-945

DOI https://doi.org/10.1248/cpb.56.941

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Abstract

A series of novel N-anilino-5-methyl-2-(3-(5-(alkylaminomethyl)furan-2-yl-methylthio)propyl)-[1,2,4]triazolo-[1,5-a]pyrimidine-7-amine derivatives were synthesized and evaluated for their in vitro cytotoxicity against two cancer cell lines, Bel-7402 and HT-1080. Compounds 9, 14, 19 and 23 possessed marked cytotoxicity, especially 23 (with IC₅₀ values of 15.0 μM and 7.8 μM against Bel-7402 and HT-1080 cell lines, respectively), which had emerged as lead compound. The activity was found to depend strongly on substitution pattern of the side chains at C-2 position, and 4-triflouromethylanilino substituent at C-7 position was an option for anticancer potency.

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